Search Results - "Kankanala, Jayakanth"

Design, Synthesis, and Biological Evaluations of Hydroxypyridonecarboxylic Acids as Inhibitors of HIV Reverse Transcriptase Associated RNase H by Kankanala, Jayakanth, Kirby, Karen A, Liu, Feng, Miller, Lena, Nagy, Eva, Wilson, Daniel J, Parniak, Michael A, Sarafianos, Stefan G, Wang, Zhengqiang

“…Targeting the clinically unvalidated reverse transcriptase (RT) associated ribonuclease H (RNase H) for human immunodeficiency virus (HIV) drug discovery…”
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Toward Structurally Novel and Metabolically Stable HIV-1 Capsid-Targeting Small Molecules by Vernekar, Sanjeev Kumar V, Sahani, Rajkumar Lalji, Casey, Mary C, Kankanala, Jayakanth, Wang, Lei, Kirby, Karen A, Du, Haijuan, Zhang, Huanchun, Tedbury, Philip R, Xie, Jiashu, Sarafianos, Stefan G, Wang, Zhengqiang

“…HIV-1 capsid protein (CA) plays an important role in many steps of viral replication and represents an appealing antiviral target. Several CA-targeting small…”
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Site-directed M2 proton channel inhibitors enable synergistic combination therapy for rimantadine-resistant pandemic influenza by Scott, Claire, Kankanala, Jayakanth, Foster, Toshana L, Goldhill, Daniel H, Bao, Peng, Simmons, Katie, Pingen, Marieke, Bentham, Matthew, Atkins, Elizabeth, Loundras, Eleni, Elderfield, Ruth, Claridge, Jolyon K, Thompson, Joseph, Stilwell, Peter R, Tathineni, Ranjitha, McKimmie, Clive S, Targett-Adams, Paul, Schnell, Jason R, Cook, Graham P, Evans, Stephen, Barclay, Wendy S, Foster, Richard, Griffin, Stephen, Lowen, Anice C, Pekosz, Andrew

“…Pandemic influenza A virus (IAV) remains a significant threat to global health. Preparedness relies primarily upon a single class of neuraminidase (NA)…”
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Discovery of N-benzyl hydroxypyridone carboxamides as a novel and potent antiviral chemotype against human cytomegalovirus (HCMV) by Senaweera, Sameera, Edwards, Tiffany C., Kankanala, Jayakanth, Wang, Yan, Sahani, Rajkumar Lalji, Xie, Jiashu, Geraghty, Robert J., Wang, Zhengqiang

“…Current drugs for treating human cytomegalovirus (HCMV) infections are limited by resistance and treatment-associated toxicities. In developing mechanistically…”
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Rationally derived inhibitors of hepatitis C virus (HCV) p7 channel activity reveal prospect for bimodal antiviral therapy by Shaw, Joseph, Gosain, Rajendra, Kalita, Monoj Mon, Foster, Toshana L, Kankanala, Jayakanth, Mahato, D Ram, Abas, Sonia, King, Barnabas J, Scott, Claire, Brown, Emma, Bentham, Matthew J, Wetherill, Laura, Bloy, Abigail, Samson, Adel, Harris, Mark, Mankouri, Jamel, Rowlands, David J, Macdonald, Andrew, Tarr, Alexander W, Fischer, Wolfgang B, Foster, Richard, Griffin, Stephen

“…Since the 1960s, a single class of agent has been licensed targeting virus-encoded ion channels, or 'viroporins', contrasting the success of channel blocking…”
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In silico design and biological evaluation of a dual specificity kinase inhibitor targeting cell cycle progression and angiogenesis by Latham, Antony M, Kankanala, Jayakanth, Fearnley, Gareth W, Gage, Matthew C, Kearney, Mark T, Homer-Vanniasinkam, Shervanthi, Wheatcroft, Stephen B, Fishwick, Colin W G, Ponnambalam, Sreenivasan

“…Protein kinases play a central role in tumor progression, regulating fundamental processes such as angiogenesis, proliferation and metastasis. Such enzymes are…”
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Receptor tyrosine kinase structure and function in health and disease by A. Karpov, Oleg, W. Fearnley, Gareth, A. Smith, Gina, Kankanala, Jayakanth, J. McPherson, Michael, C. Tomlinson, Darren, A. Harrison, Michael, Ponnambalam, Sreenivasan

“…Receptor tyrosine kinases (RTKs) are membrane proteins that control the flow of information through signal transduction pathways, impacting on different…”
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Isoquinoline-1,3-diones as Selective Inhibitors of Tyrosyl DNA Phosphodiesterase II (TDP2) by Kankanala, Jayakanth, Marchand, Christophe, Abdelmalak, Monica, Aihara, Hideki, Pommier, Yves, Wang, Zhengqiang

“…Tyrosyl DNA phosphodiesterase II (TDP2) is a recently discovered enzyme that specifically repairs DNA damages induced by topoisomerase II (Top2) poisons and…”
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Novel deazaflavin tyrosyl-DNA phosphodiesterase 2 (TDP2) inhibitors by Kiselev, Evgeny, Ravji, Azhar, Kankanala, Jayakanth, Xie, Jiashu, Wang, Zhengqiang, Pommier, Yves

“…•Novel deazaflavin derivative ZW-1288 is a potent inhibitor of recombinant and cellular human TDP2.•ZW-1288 specifically potentiates cytotoxic action of the…”
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5′-Silylated 3′-1,2,3-triazolyl Thymidine Analogues as Inhibitors of West Nile Virus and Dengue Virus by Vernekar, Sanjeev Kumar V, Qiu, Li, Zhang, Jing, Kankanala, Jayakanth, Li, Hongmin, Geraghty, Robert J, Wang, Zhengqiang

“…West Nile virus (WNV) and Dengue virus (DENV) are important human pathogens for which there are presently no vaccine or specific antivirals. We report herein a…”
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Inhibition of Human Cytomegalovirus pUL89 Terminase Subunit Blocks Virus Replication and Genome Cleavage by Wang, Yan, Mao, Lili, Kankanala, Jayakanth, Wang, Zhengqiang, Geraghty, Robert J

“…The human cytomegalovirus terminase complex cleaves concatemeric genomic DNA into unit lengths during genome packaging and particle assembly. This process is…”
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Design, Synthesis, Biochemical, and Antiviral Evaluations of C6 Benzyl and C6 Biarylmethyl Substituted 2‑Hydroxylisoquinoline-1,3-diones: Dual Inhibition against HIV Reverse Transcriptase-Associated RNase H and Polymerase with Antiviral Activities by Vernekar, Sanjeev Kumar V, Liu, Zheng, Nagy, Eva, Miller, Lena, Kirby, Karen A, Wilson, Daniel J, Kankanala, Jayakanth, Sarafianos, Stefan G, Parniak, Michael A, Wang, Zhengqiang

“…Reverse transcriptase (RT) associated ribonuclease H (RNase H) remains the only virally encoded enzymatic function not targeted by current chemotherapy against…”
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Hydroxypyridonecarboxylic Acids as Inhibitors of Human Cytomegalovirus pUL89 Endonuclease by Kankanala, Jayakanth, Wang, Yan, Geraghty, Robert J., Wang, Zhengqiang

“…Human cytomegalovirus (HCMV) infection poses a major health threat to immunocompromised individuals. Until recently, treatment of HCMV infection has relied…”
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Triazolopyrimidine and triazolopyridine scaffolds as TDP2 inhibitors by Ribeiro, Carlos J.A., Kankanala, Jayakanth, Xie, Jiashu, Williams, Jessica, Aihara, Hideki, Wang, Zhengqiang

“…[Display omitted] •Four derivatives possess significant TDP2 inhibition (IC50 < 50 µM).•17z (IC50 of 21.0 ± 2.1 µM) shows excellent cell permeability and no…”
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Design, synthesis and biological evaluations of N-Hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H by Kankanala, Jayakanth, Kirby, Karen A., Huber, Andrew D., Casey, Mary C., Wilson, Daniel J., Sarafianos, Stefan G., Wang, Zhengqiang

“…Human immunodeficiency virus (HIV) reverse transcriptase (RT) associated ribonuclease H (RNase H) is the only HIV enzymatic function not targeted by current…”
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3‑Hydroxypyrimidine-2,4-dione-5‑N‑benzylcarboxamides Potently Inhibit HIV‑1 Integrase and RNase H by Wu, Bulan, Tang, Jing, Wilson, Daniel J, Huber, Andrew D, Casey, Mary C, Ji, Juan, Kankanala, Jayakanth, Xie, Jiashu, Sarafianos, Stefan G, Wang, Zhengqiang

“…Resistance selection by human immunodeficiency virus (HIV) toward known drug regimens necessitates the discovery of structurally novel antivirals with a…”
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Novel Deazaflavin Analogues Potently Inhibited Tyrosyl DNA Phosphodiesterase 2 (TDP2) and Strongly Sensitized Cancer Cells toward Treatment with Topoisomerase II (TOP2) Poison Etoposide by Kankanala, Jayakanth, Ribeiro, Carlos J. A, Kiselev, Evgeny, Ravji, Azhar, Williams, Jessica, Xie, Jiashu, Aihara, Hideki, Pommier, Yves, Wang, Zhengqiang

“…Topoisomerase II (TOP2) poisons as anticancer drugs work by trapping TOP2 cleavage complexes (TOP2cc) to generate DNA damage. Repair of such damage by tyrosyl…”
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5-Aminothiophene-2,4-dicarboxamide analogues as hepatitis B virus capsid assembly effectors by Tang, Jing, Huber, Andrew D., Pineda, Dallas L., Boschert, Kelsey N., Wolf, Jennifer J., Kankanala, Jayakanth, Xie, Jiashu, Sarafianos, Stefan G., Wang, Zhengqiang

“…Chronic hepatitis B virus (HBV) infection represents a major health threat. Current FDA-approved drugs do not cure HBV. Targeting HBV core protein (Cp)…”
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Repurposing N-hydroxy thienopyrimidine-2,4-diones (HtPD) as inhibitors of human cytomegalovirus pUL89 endonuclease: Synthesis and biological characterization by He, Tianyu, Edwards, Tiffany C., Majima, Ryuichi, Jung, Eunkyung, Kankanala, Jayakanth, Xie, Jiashu, Geraghty, Robert J., Wang, Zhengqiang

“…[Display omitted] •Metal-chelating HIV RNase H inhibitors repurposed as HCMV pUL89-C inhibitors.•New isomeric N-hydroxy thienopyrimidine-2,4-dione (HtPD)…”
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New fluorescence-based high-throughput screening assay for small molecule inhibitors of tyrosyl-DNA phosphodiesterase 2 (TDP2) by Ribeiro, Carlos J.A., Kankanala, Jayakanth, Shi, Ke, Kurahashi, Kayo, Kiselev, Evgeny, Ravji, Azhar, Pommier, Yves, Aihara, Hideki, Wang, Zhengqiang

“…Tyrosyl-DNA phosphodiesterase 2 (TDP2) repairs topoisomerase II (TOP2) mediated DNA damages and causes resistance to TOP2-targeted cancer therapy. Inhibiting…”
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